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A Novel Sarsolenane Diterpene as a PTP1B Inhibitor from Hainan Soft Coral Sarcophyton trocheliophorum Marenzeller
Abstract:A novel sarsolenane diterpene, named secodihydrosarsolenone ( 1 ), as a minor component was obtained from the South China Sea soft coral Sarcophyton trocheliophorum Marenzeller. Its structure was elucidated by detailed spectroscopic analysis. Compound 1 exhibited moderate inhibitory activity (IC50 =13.7 µmol•L−1) against protein tyrosine phosphatase 1B (PTP1B ), a key target for the treatment of type 2 diabetes, representing the first report of PTP1B inhibitory activity for sarsolenane diterpenes. This discovery promotes computational prediction of binding mode between the enzyme and the metabolite, suggesting a crucial role of the residues Tyr46, Ser216 and Arg221 in the binding action.
Keywords:Sarcophyton trocheliophrum  sarsolenane  structure elucidation  PTP1B inhibitory activity  binding mode
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